Human ABC Transporter ABCG2 in Cancer Chemotherapy: Drug Molecular Design to Circumvent Multidrug Resistance

  • Toshihisa IshikawaEmail author
  • Hikaru Saito
  • Hiroyuki Hirano
  • Yutaka Inoue
  • Yoji Ikegami
Part of the Methods in Molecular Biology book series (MIMB, volume 910)


Human ATP-binding cassette (ABC) transporter ABCG2 (BCRP) is critically involved in multidrug resistance of human cancer. This transporter exhibits broad substrate specificity toward structurally diverse compounds, as do other ABC transporters, such as ABCB1 (P-glycoprotein/MDR1), ABCC1 (MRP1/GS-X pump), and ABCC2 (MRP2/cMOAT). To gain insight into the relationship between the molecular structure of compounds and the ABCG2-mediated transport activity, we have developed a high-speed screening method to analyze the substrate specificity of ABCG2. In addition, we have developed an algorithm that analyzes QSAR to evaluate ABCG2–drug interactions. This chapter presents our strategy of transport mechanism-based molecular design to circumvent multidrug resistance of cancer.

Key words

ABC transporter ABCG2 (BCRP) Cancer Protein kinase inhibitor Quantitative ­structure–activity relationship (QSAR) 


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Copyright information

© Springer Science+Business Media New York 2012

Authors and Affiliations

  • Toshihisa Ishikawa
    • 1
    Email author
  • Hikaru Saito
    • 1
    • 2
  • Hiroyuki Hirano
    • 1
  • Yutaka Inoue
    • 3
  • Yoji Ikegami
    • 3
  1. 1.Graduate School of Bioscience and BiotechnologyTokyo Institute of TechnologyYokohamaJapan
  2. 2.Oral Formulation Development, Pharmaceutical Research and Technology LaboratoriesAstellas Pharma IncShizuokaJapan
  3. 3.Department of Drug Metabolism and DispositionMeiji Pharmaceutical UniversityTokyoJapan

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